Synthesis, characterization and high in vitro antitumour activity of novel triphenyltin carboxylates

The synthesis and spectral characterization of six novel triphenyltin compounds are described. The in vitro antitumour activity of three of these compounds against two human tumour cell lines, MCF-7, a mammary tumour, and WiDr, a colon carcinoma, was determined. All three compounds are more active than cis-platin, etoposide and doxorubicin against both tumour cell lines. They are as active as mitomycin C against WiDr, but less active against MCF-7.     

Synthesis,characterization and antitumour studies of metal chelates of N1-isonicotinoyl-3-methyl-4-(p-hydroxybenzilidene)-2-pyrazolin-5-one

The cobalt(II), nickel(II) and copper(II) complexes of N-Isonicotinoyl-3-methyl-4-(p-hydroxybenzilidene)-2-pyrazolin-5-one (IMHBP) with different counter anions have been prepared and characterized. An octahedral geometry has been assigned to the cobalt(II) and nickel(II) complexes and a square-planar structure to the copper(II) complexes. IMHBP acts as a neutral bidentate ligand in all these complexes by coordinating through the oxygen atoms of the amide group and carbonyl at position-5. The other coordination sites are satisfied by anions alone or anions and water molecules. The ligand and the complexes were screened for their possible antitumour activity. The copper(II) complexes are appreciably active in reducing mice tumours.     

1,2,3,4-丁烷四羧酸过渡金属配合物的制备和表征

用过渡金属盐与 1,2 ,3,4 -对所制金属配合物的组成和结构进行了表征。利用热重分析对该配合物的热稳定性进行了研究 ,得出其热稳定性次序为 :Cu2 C8H6O8相似文献   

稀土三元配合物的合成、表征及其抗菌活性研究

以稀土氯化物、联咪唑和噻吩甲酰三氟丙酮为原料制备了一系列新型稀土三元配合物Ln(TTA)3L(Ln=Nd3+,Eu3+,Er3+;TTA=噻吩甲酰三氟丙酮;L=联咪唑),抗菌实验结果显示,三元配合物抑菌圈直径为12～17 mm,对大肠杆菌、金黄色葡萄球菌具有一定的抑制作用,且对大肠杆菌的抑制效果较好。     

钇三元配合物的合成、表征及其抗菌活性研究

以YCl3.6H2O、2,6-吡啶二羧酸(PDA)和噻吩甲酰三氟丙酮(TTA)为原料,制备了钇的三元配合物,用元素分析、红外光谱、X射线光电子能谱对配合物进行了表征,确定了配合物的化学组成为:Na[Y(TTA)2(PDA)].3H2O(反应时间为1 h)和Na2[Y(TTA)3(PDA)].3H2O(反应时间为0.5 h)。抗菌实验表明,Na[Y(TTA)2(PDA)].3H2O对大肠杆菌和金黄色葡萄球菌的抑菌圈直径分别约为14,12 mm,Na2[Y(TTA)3(PDA)].3H2O分别约为16,14 mm,说明配合物对大肠杆菌、金黄色葡萄球菌具有一定的抑制作用,且对大肠杆菌的抑制效果较好。     

6-丙基-2-硫尿嘧啶的合成

在无水氯化镁、三乙胺存在下,丁酰氯与丙二酸单乙酯钾盐经缩合、酸解得到丁酰乙酸乙酯;然后与硫脲经脱水、缩合成环后得到6-丙基-2-硫脲嘧啶.结构经1H NMR、IR和MS表征.最佳反应条件为:n(硫脲)/n(丁酰乙酸乙酯)/n(氢氧化钾)=1.00/2.30/2.30时,产物收率为84.71％.本工艺反应条件温和,操作简单,收率高,适合工业化生产.     

Synthesis,characterization, and thermal stability of azomethine oligomer and its metal complexes

The oxidative polycondensation reaction conditions of N,N′‐bis[(2‐hydroxy‐1‐naphthyl)methylene]urea (2‐HNMU) has been accomplished using NaOCl, H₂O₂, and air O₂ oxidants in an aqueous alkaline medium. The structures of the obtained monomer and oligomer were confirmed by FTIR, UV–vis, ¹H NMR, ¹³C NMR, and elemental analysis. The characterization was made by TG‐DTA, size exclusion chromatography (SEC), and solubility tests. At the optimum reaction conditions, the yield of oligo‐N,N′‐bis[(2‐hydroxy‐1‐naphthyl)methylene]urea (O‐2‐HNMU) was found to be 95% (for air O₂ oxidant), 51% (for H₂O₂ oxidant), 96% (for NaOCl oxidant). According to the SEC analysis, the number‐average molecular weight (M_n), weight‐average molecular weight (M_w), and polydispersity index values of O‐2‐HNMU was found to be 1036, 1225 g/mol, and 1.182, respectively, using H₂O₂, and 765, 1080 g/mol, and 1.412, respectively, using air O₂, and 857, 1105 g/mol, and 1.289, respectively, using NaOCl. TG‐DTA analyses showed that O‐2‐HNMU was more stable than 2‐HNMU. According to TG analyses, the carbonaceous residue of 2‐HNMU and O‐2‐HNMU was found to be 0.49% and 2.11% at 1000°C, respectively. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2007     

含硫双Schiff碱及其金属配合物的合成、表征与生物活性研究

合成了茚三酮-1,3-双缩肼基二硫代甲酸苄酯(HL1),茚三酮-1,3-双缩氨基硫脲(HL2)两种含硫双Schiff碱及它们的铜、钴金属等配合物,通过元素分析、红外光谱、紫外-可见光谱、差热和摩尔电导等测试对其进行了表征,并测试了双Schiff碱配体与金属配合物对大肠杆菌、枯草芽孢杆菌的抑菌活性。     

Synthesis and antifungal activity of metal complexes containing dichloro-tetramorpholino-cyclophosphazatriene

Metal complexes of dichloro-tetramorpholino-cyclophosphazatriene containing divalent cations such as Ni(II), Co(II), and Mn(II) have been prepared and characterised by standard physico-chemical procedures (elemental chemical analysis, IR and UV-VIS spectra, conductimetric measurement). The newly synthesised compounds possessed antifungal activity against Aspergillus and Candida spp., some of them showing effects comparable to ketoconazole (with minimum inhibitory concentrations in the range of 2- 30 mug/mL) but being generally less active as compared to the azole. Best activity was detected against C. albicans, and worst activity against A. niger. The mechanism of action of these compounds probably involves inhibition of ergosterol biosynthesis, and interaction with lanosterol-14-alpha-demethylase (CYP51A1), since reduced amounts of ergosterol were evidenced by means of HPLC in cultures of the sensitive strain A. niger treated with some of these inhibitors.     

一种新型缩氨基硫脲及其金属配合物的合成、表征与生物活性研究

合成了1-(2-羟基-1-亚甲基)-4-苯基氨基硫脲配体(HL)及它们的铜、钴、镍金属配合物,通过核磁、元素分析、摩尔电导、红外光谱、紫外-可见光谱等测试对其进行了结构表征,并测试了该配体及其金属配合物对大肠杆菌、金黄色葡萄球菌、欧文氏草生杆菌的抑菌活性。     

Synthesis, characterization, and hydrotreating activity of carbon-supported transition metal phosphides

A series of nickel, molybdenum, and tungsten metal phosphides deposited on a carbon black support (Ni₂P/C, MoP/C, and WP/C) were synthesized by means of temperature-programmed reduction. The samples were characterized by BET surface area, CO uptake, X-ray diffraction (XRD), elemental analysis, and extended X-ray absorption fine structure (EXAFS) measurements. The activity of these catalysts was measured at 613 K and 3.1 MPa in a three-phase, packed-bed reactor for hydrodesulfurization (HDS) and hydrodenitrogenation (HDN) with a model liquid feed containing 500 ppm sulfur as 4,6-dimethyldibenzothiophene (4,6-DMDBT), 3000 ppm sulfur as dimethyl disulfide, and 200 ppm nitrogen as quinoline. The Ni₂P/C catalyst was found to exhibit the best hydroprocessing performance based on equal CO chemisorption sites (70 μmol) loaded in the reactor. An optimum Ni loading for HDS and HDN activity was found as 1.656 mmol g⁻¹ (11.0 wt.% Ni₂P) which gave an HDS conversion of 99% and an HDN conversion of 100% at a molar space velocity of 0.88 h⁻¹. These were much higher than those of a commercial Ni-Mo-S/γ-Al₂O₃ catalyst which gave an HDS conversion of 68% and an HDN conversion of 94%, and a previously reported best Ni₂P/SiO₂ catalyst which gave an HDS conversion of 76% and an HDN conversion of 92%. The use of carbon instead of silica as a support gave rise to other differences, which included smaller particle size, higher CO uptake, lessened retention of P on the support, and reduced sulfur deposition. The stability of the 11.0 wt.% Ni₂P/C catalyst was also excellent with no deactivation observed over 110 h of time on stream. The activity and stability of the Ni₂P/C catalyst were affected by the phosphorous content, both reaching a maximum with an initial Ni/P ratio of 1/2. EXAFS and elemental analysis of the spent samples indicated the formation of a surface phosphosulfide phase on the Ni₂P, which was beneficial for hydrotreating activity, while the bulk structure of the phosphides was maintained during the course of reaction as revealed from the XRD patterns.     

Metal-5-Fluorouracil-histamine complexes: solution, structural, and antitumour studies

Solution studies were performed pH-metrically to study the interaction of Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) metal ions with 5-fluorouracil (5FU) and histamine (Hm) separately (binary) and in the presence of each other (ternary) at 25+/-0.1( degrees )C temperature and a constant ionic strength of 0.1 M NaNO(3) in aqueous solution. The ternary complexes have been found to be more stable than the corresponding binary complexes as shown by the positive value of DeltalogK. The species distribution curves have been obtained using the computer programme BEST. On the basis of species distribution results, efforts were also made to prepare some mixed complexes of Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) ions by performing the reaction of their metal nitrates, 5FU and Hm in aqueous ethanol medium at suitable pH. The isolated solid complexes were characterized by different physico-chemical method in order to suggest the possible binding site of the ligands and the structure of the resultant complexes. All these complexes were checked for their antitumour activity by injecting in Dalton's lymphoma (DL) and Sarcoma-180 (S-180) bearing C(3)H/He mice. The results indicate that some complexes have good antitumour activity both in vivo and in vitro.     

一种新型酰腙金属配合物的合成及其晶体表征

基于酰腙类及其配合物较强的生物活性及稳定性,设计了5-溴-2-羟基苯基乙酮对羟基苯甲酰腙的合成路线,并使之与金属铜离子反应,合成了一种新的金属配合物（Sehiff碱配合物）5-溴-2-羟基苯基乙酮对羟基苯甲酰腙合铜配合物。培养成单晶后通过x-射线单晶衍射对其结构进行了表征,结果表明,该酰腙分子具有较高的配位能力、生物活性和化学稳定性。     

安息香缩氨基硫脲及其配合物的合成,表征和生物活性研究

合成了安息香缩氨基硫脲及其与Ｃｕ（Ⅱ），Ｍｎ（Ⅱ），Ｚｎ（Ⅱ），Ｎｉ（Ⅱ），Ｃｏ（Ⅱ）的配合物，通过元素分析，摩尔电导率，磁化率，紫外光谱和红外光谱等进行了表征。测定了配体及配合物的生物活性。实验发现，配体无抗菌活性，形成配合物后具有抗菌活性。     

Chitosan- metal complexes as antimicrobial agent: Synthesis, characterization and Structure-activity study

Summary Chitosan (CS) metal complexes with bivalent metal ions, including Cu(II), Zn(II), Fe(II) were prepared, and characterized by FT-IR, XRD, AAS and elemental analysis. The crystalline and structural properties of chitosan-metal complexes were different from those of chitosan, and the -NH₂, -OH groups in chitosan molecule were considered as the dominating reactive sites. In vitro antimicrobial activities of the obtained chitosan-metal complexes, which were found to be much better than free chitosan and metal salts, were examined against two gram-positive bacteria (S. aureus and S. epidermidis), two gram-negative bacteria (E. coli and P. aeruginosa) and two fungi (C. albicans and C. parapsilosis). Results indicatd that the inhibitory effects of chitosan-metal complexes were dependent on the property of metal ions, the molecular weight and degree of deacetylation of chitosan and environmental pH values. Electro microscopy confirmed that the exposure of S. auresus to the chitosan-Cu(II) complex resulted in the disruption of cell envelop. Based on the discussion upon the antimicrobial mechanism of chitosan-metal complexes and their molecular structures, the structure-activity correlation for the antimicrobial activities was elucidated. All the results show that chitosan-metal complexes are a promising candidate for novel antimicrobial agents that can be used in cosmetic, food, textile et al.     

硫代磷酰二腙及其配合物的合成和生物活性

合成了一种硫代磷酰二腙配体(H2L)及其Mn(Ⅱ)、Fe(Ⅱ)、Co(Ⅱ)配合物,所合成的配体及配合物均用元素分析、摩尔电导、UV、IR等手段进行了表征,对配体还用MS和1HNMR进行了结构表征。测定了化合物的杀虫活性以及对水稻幼苗细胞超氧化物歧化酶(SOD)活力的影响,表明这些化合物具有一定杀虫活性并能激活水稻细胞SOD。     

Synthesis, characterization and antitumor activity of a series of polypyridyl complexes

A series of polypyridyl complexes have been synthesized. All polypyridyl complexes and some of the soluble ligands have been assayed for antitumor activity in vitro against the HL-60 (the human leucocytoma) cells, BEL-7402 (the human liver carcinoma) cells, KB (the human nasopharyngeal carcinoma) cells and HELA (the human adenocarcinoma of cervix) cells. The results indicate that several complexes have relative activity against different cell lines. Especially, the complexes [Co(bpy)(2)(pip)](3+), [Co(phen)(2)(pip)](3+), [Ru(bpy)(2)(pztp)](2+) and [Ru(pztp)(2)(bpy)](2+) show relative high activity against four tumor cell lines. Moreover, they are slightly more effective than cisplatin. At the concentration of 100 mug/mL, the complexes show inhibitory rate of 72 approximately 86% for the cancer cells and have no toxicity for MDCK and Vero cells. It is indicated that these complexes can inhibit cancer cells selectively.     

2-(3-羧基-2,4,5-三氮唑偶氮)-5-乙酰氨基苯酚的合成及其与钴的显色反应研究

合成了新试剂 2 -(3 -羧基 -2 ,4,5 -三氮唑偶氮 ) -5 -乙酰氨基苯酚 (CTZAAP) ,并研究了其与钴的显色反应及应用。在 p H7.61的 Na H2 PO4 -Na2 HPO4 缓冲液中该试剂与钴形成 2∶ 1红色稳定配合物 ,λmax为 5 2 9.2 nm,钴量在 0～ 1 .2 μg·m L- 1 范围内符合比尔定律 ,表观摩尔吸光系数为 4.61× 1 0 4 L· mol- 1 · cm- 1 。方法用于维生素 B1 2 注射液及环境水样中的微量钴测定 ,结果满意     

2-羟基-1-萘醛缩乙二胺Schiff碱及其稀土金属配合物的合成和表征

以2-羟基-1-萘醛和乙二胺为原料,乙醇为溶剂,加热回流制备2-羟基-1-萘醛缩乙二胺Schiff碱配体,然后分别与铟（Ⅲ）、钍（Ⅳ）的盐反应,生成相应的配合物,并对2-羟基-1-萘醛缩乙二胺Schiff碱及其金属配合物的抗菌活性进行探究。结果表明,配合物对枯草杆菌、大肠杆菌、绿脓杆菌和金黄色葡萄球菌的抑制作用较配体更强。     

缩聚活性的铽配合物合成、表征及其性质

通过HCl气体在无水乙醇中,与Tb4O7反应生成无水TbCl3,再与具有胺基的配体反应,合成了一种两端带有胺基的呈缩聚活性的铽配合物。用元素分析、红外光谱和紫外光谱对配合物的组成和结构进行了表征,并借摩尔电导、差热-热重和荧光光谱对配合物进行了研究。配合物的起始分解温度为230℃左右,粉末状态下具有较高的荧光强度,单色性好,在DMF中可作为聚合单体应用。